Abstract: This invention relates to compounds that inhibit or modulate the activity of Chk-1 kinase. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds.
Type:
Grant
Filed:
March 3, 2021
Date of Patent:
October 17, 2023
Assignee:
SENTINEL ONCOLOGY LIMITED
Inventors:
Robert George Boyle, David Winter Walker, Richard Justin Boyce, Scott Peterson, Francine Farouz, Cong Hung Vo
Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of retinoids and retinoid-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
Abstract: The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.
Type:
Grant
Filed:
August 31, 2021
Date of Patent:
October 10, 2023
Assignee:
EMORY UNIVERSITY
Inventors:
Michael G. Natchus, Richard Arrendale, Dennis C. Liotta, Ketan Desai, Hyunsuk Shim
Abstract: Methods of treating tinnitus, acute sensorineural hearing loss, Meniere's disease, Tourette's syndrome, ADHD or addiction with (1S,3S)-3-amino-4-(difluoromethylidene) cyclopentane-1-carboxylic acid or a pharmaceutically acceptable salt thereof are provided. Methods of treating tinnitus, acute sensorineural hearing loss, Meniere's disease, Tourette's syndrome, ADHD or addiction with (S)-3-amino-4-(difluoromethylenyl)cyclopent-1-ene-1-carboxylic acid are provided. Also provided are therapeutic compositions that may be used to improve one or more symptoms of tinnitus, acute sensorineural hearing loss, Meniere's disease, Tourette's syndrome, ADHD or addiction.
Abstract: Disclosed herein are compositions comprising an NSAID such as meloxicam and/or rizatriptan in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tmax of meloxicam of 3 hours or less.
Abstract: This invention provides new methods for a) identifying Cushing's Syndrome patients at high risk of developing hypokalemia during glucocorticoid receptor modulator (GRM) treatment, and b) for prophylactically treating such patients to prevent, or reduce the severity of, hypokalemia. Patients at such high risk may be identified prior to their developing hypokalemia. Such a patient may be an adult patient with endogenous Cushing's Syndrome having type 2 diabetes mellitus or glucose intolerance to control hyperglycemia secondary to hypercortisolism. Patients may be identified by an above-threshold level of ACTH or cortisol in a patient sample taken post-GRM administration or pre-GRM administration, respectively. Upon identifying such a patient prior to the development of low potassium, the present methods provide for prophylactically treating the patient by administration of one or more hypokalemia treatments concurrently with an increased dose of GRM or with an initial dose of GRM to prevent hypokalemia.
Abstract: The present invention regards specific IBAT inhibitors useful in the prophylaxis and/or treatment of a liver disease. It also relates to compositions comprising these IBAT inhibitors, a method for treatment of the disorders and a kit comprising the substances or the compositions.
Type:
Grant
Filed:
March 19, 2021
Date of Patent:
August 22, 2023
Assignee:
Albireo AB
Inventors:
Per-Göran Gillberg, Hans Graffner, Ingemar Starke
Abstract: An embodiment relates to a crystal polymorph of 8-bromo-2-(1-methylpiperidin-4-ylamino)-4-(4-phenoxyphenylamino)pyrido [4,3-d]pyrimidin-5(6H)-one hydrochloride which can effectively suppress FLT3 and has excellent stability even in a high temperature and humid environment, and a method for preparing same.
Type:
Grant
Filed:
August 12, 2019
Date of Patent:
August 22, 2023
Assignee:
OSCOTEC INC.
Inventors:
Jung-Ho Kim, Jang-Sik Choi, Hee Kyu Lee, Song-eun Park, Dong-Sik Jung, Yung-Geun Choi, Jong-Sung Koh, Se-Won Kim, Jaekyoo Lee
Abstract: The present invention relates to compounds of Formula I as defined herein, and salts and solvates thereof. (I) The present invention also relates to pharmaceutical compositions comprising compounds of Formula (I), and to compounds of Formula (I) for use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which inhibition of a RAS-effector protein-protein interaction is implicated.
Type:
Grant
Filed:
January 23, 2019
Date of Patent:
August 15, 2023
Assignee:
OXFORD UNIVERSITY INNOVATION LIMITED
Inventors:
Terrence Rabbitts, Camilo Quevedo, Abimael Cruz, Simon Phillips, Philip Spencer Fallon, Anna Hopkins, Lydia Yuen-Wah Lee, Tenin Traore, Sophie Caroline Williams, Natalie Louise Winfield
Abstract: The invention provides compounds having STimulator of INterferon Genes (STING) agonistic bioactivity that can be used in the treatment of tumors in patients afflicted therewith. The compounds are of formula (I): as defined herein. Compounds for practice of a method of the invention can be delivered via oral delivery for systemic exposure, as well as delivered intratumorally. Antitumor therapy using a compound of formula (I) can further comprise administration of an effective dose of an immune-checkpoint targeting drug.
Type:
Grant
Filed:
February 21, 2019
Date of Patent:
July 18, 2023
Assignee:
The Scripps Research Institute
Inventors:
Luke L. Lairson, Emily Chin, Arnab K. Chatterjee, Manoj Kumar, Ana Maria Gamo Albero, Hank Michael James Petrassi, Peter G. Schultz, Chenguang Yu, Junko Tamiya, William Vernier, Anil Gupta, Ramkumar Modukuri
Abstract: This disclosure provides a method of safely and rapidly initiating or escalating oral sotalol therapy by administering an intravenous dosage of sotalol followed by oral sotalol twice daily.
Type:
Grant
Filed:
November 24, 2019
Date of Patent:
July 11, 2023
Assignee:
AltaThera Pharmaceuticals, LLC
Inventors:
John Somberg, Brandon Ira Kashfian, Janos Molnar
Abstract: The present disclosure provides, inter alia, methods of treating generalized pustular psoriasis (GPP) by administering an effective amount of a Chemokine Receptor 6 (CCR6) antagonist and/or a C-X-C motif chemokine receptor 2 (CXCR2) antagonist. Also provided herein are methods of modulating dysregulated IL-36 signaling in a subject in need thereof and methods of reducing neutrophil, inflammatory dendritic cell (iDC), and/or CD4 T cell accumulation in a subject in need thereof, said methods, include dministering an effective amount of a Chemokine Receptor 6 (CCR6) antagonist and/or a C-X-C motif chemokine receptor 2 (CXCR2) antagonist.
Type:
Grant
Filed:
November 16, 2021
Date of Patent:
June 27, 2023
Assignee:
CHEMOCENTRYX, INC.
Inventors:
James J. Campbell, Karen Ebsworth, Antoni Krasinski, Venkat Reddy Mali, Jeffrey McMahon, Rajinder Singh, Ju Yang, Chao Yu, Penglie Zhang
Abstract: This disclosure relates to managing conditioned fear and conditions induced by experiencing or witnessing an extreme traumatic event using neurokinin receptor antagonists. In certain embodiments, the disclosure relates to methods of treating or preventing conditioned fear comprising administering an effective about neurokinin 3 receptor antagonist to a subject in need thereof. In certain embodiments, the subject is diagnosed with Post-Traumatic Stress Disorder.
Abstract: Novel cromolyn analogs useful as imaging agents for detecting atherosclerotic plaques and for treating atherosclerosis and Alzheimer's Disease, and methods of making the cromolyn analogs, are disclosed. The cromolyn analogs have the general formula: wherein X is OH, C1-C6 alkoxyl; Y and Z are independently selected from a C1-C6 alkyl, C1-C6 alkoxyl, halogen, un-substituted or C1-C6 substituted amine, 18F, 19F, or H; and n is 1, 2, or 3; and wherein for structure (I), if n are both 1 and Y and Z are both H and X is OH.
Abstract: Provided are methods of administering a vesicular monoamine transport 2 (VMAT2) inhibitor chosen from valbenazine and (+)-?-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,1 1b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol, or a pharmaceutically acceptable salt and/or isotopic variant thereof, to a patient in need thereof wherein the patient is also being administered digoxin.
Type:
Grant
Filed:
October 20, 2020
Date of Patent:
May 23, 2023
Assignee:
Neurocrine Biosciences, Inc.
Inventors:
Christopher F. O'Brien, Haig P. Bozigian
Abstract: Pharmaceutical compositions of colchicine for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined or desired release profile. Methods of treating or preventing cardiovascular disease and/or inflammatory disease in mammalian subjects comprising the administration of the novel formulations disclosed herein are also provided.
Abstract: The invention relates generally to a silvestrol molecule activated with a leaving group. The invention further relates generally to an antibody-drug conjugate comprising an antibody conjugated by a linker to one or more silvestrol drug moieties and methods of treatment.
Type:
Grant
Filed:
March 23, 2020
Date of Patent:
May 16, 2023
Assignee:
Genentech, Inc.
Inventors:
Thomas Pillow, Andrew G. Polson, Bing Zheng